In addition to its stimulant effects, mephedrone produces side effects, of which teeth grinding is the most common. The metabolism of mephedrone has been studied in rats and humans and the metabolites can be detected in urine after usage.

Mephedrone was first synthesised in 1929, but did not become widely known until it was rediscovered in 2003 at which point it was legal to produce and possess in many countries. By 2007, mephedrone was reported to be available for sale on the internet, by 2008 law enforcement agencies had become aware of the compound, and by 2010, it had been reported in most of Europe, becoming particularly prevalent in the United Kingdom.

Mephedrone was first made illegal in Israel in 2008, followed by Sweden later that year. In 2010, it was made illegal in many European countries and in December 2010, the EU ruled it illegal. In Australia, New Zealand and the United States, it is considered an analog of other illegal drugs and can be controlled by laws similar to the USFederal Analog Act. In September 2011, the US temporarily classified mephedrone as a Schedule I drug, effective October 2011. This classification was made permanent in July 2012 with the passage of the Synthetic Drug Abuse Prevention Act (SDAPA).